The present invention relates to taxane compounds possessing strong anti-tuberculosis activity, compositions including these compounds, processes for synthesizing these compounds, and methods for treating patients suffering from tuberculosis.
Tuberculosis is the leading cause of death in the world from a infectious disease. The cause of tuberculosis is the bacterium Mycobacterium tuberculosis (MTB), and most commonly infects the respiratory system. Tuberculosis patients have been traditionally been prescribed a course of drug treatment to eliminate MTB from the patient's body.
However, drug resistance of MTB has been become an increasing problem. Drug resistance to MTB arises due to the improper use of antibiotics in chemotherapy of drug-susceptible tuberculosis patients. This improper use is a result of a number of actions, including administration of improper treatment regimens by health care workers and failure to ensure that patients complete the whole course of treatment.
One group of compounds which has shown much promise for the treatment of tumors is the taxane group. Two prominent members of the taxane group are paclitaxel (Taxol) and docetaxel (Taxotere). Their structures are shown below:

For example, a taxane derivative identified in Taraboletti et al., Clin. Canc. Res. Vol. 8, 1182-88, April 2002, as possessing antiangiogenic and antitumor activity is IDN 5390:

However, taxanes have not previously been shown to possess anti-tuberculosis activity. Accordingly, there is a need for the development of novel anti-tuberculosis taxanes that are effective against both sensitive and resistant MTB strains.